反应详情

Heat a mixture of 3,3-dimethylcyclobutanecarboxylic acid (0.230 g, 1.792 mmol), 2-fluoro-4-methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (0.30 g, 1.195 mmol), triethylamine (TEA) (0.331 mL, 2.389 mmol) and diphenylphosphoryl azide (DPPA) (0.519 mL, 2.389 mmol) in dioxane (10 mL) at 100° C. for 2 h. Cool the mixture to RT, concentrate to dryness and purify via silica gel chromatography (10-100% EtOAc/Hexanes) to afford the title compound (220 mg, 49% yield). MS (m/z): 377.2 (M+1).

1. temperatureHeat
2. concentrationconcentrate to dryness
3. custompurify via silica gel chromatography (10-100% EtOAc/Hexanes)